Author: Gianpiero Pescarmona
Date: 02/07/2009


IDO inhibitors

Agents that interfere with tumoral immune tolerance may be useful to prevent or treat cancer. Brassinin is a phytoalexin, a class of natural products derived from plants that includes the widely known compound resveratrol. Brassinin has been demonstrated to have chemopreventive activity in preclinical models but the mechanisms underlying its anticancer properties are unknown. Here, we show that brassinin and a synthetic derivative 5-bromo-brassinin (5-Br-brassinin) are bioavailable inhibitors of indoleamine 2,3-dioxygenase (IDO), a pro-toleragenic enzyme that drives immune escape in cancer

A key in vivo antitumor mechanism of action of natural product-based brassinins is inhibition of indoleamine 2,3-dioxygenase. 2008

Structure-activity study of brassinin derivatives as indoleamine 2,3-dioxygenase inhibitors. 2006

Pharmacological targeting of IDO-mediated tolerance for treating autoimmune disease. 2007

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